pf 429242 dihydrochloride

PF-429242 is a competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). It is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO c

MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active. Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID:26617966

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P (IC50 of 175 nM).

PF-3758309 dihydrochloride is a potent, reversible, orally active, ATP-competitive PAK4 inhibitor with a Kd value of 2.7 nM and a Ki value of 18.7 nM. PF-3758309 dihydrochloride exhibits the expected cellular functions of a PAK4 inhibitor, with the ability to inhibit anchorage independent growth, induction of apoptosis, cytoskeletal remodelling and inhibition of proliferation.